| 产品描述： | XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain |
| 靶点： |
IC50: 3 nM (NaV1.7) |
| 体外研究： |
XEN907 is not cytotoxic in HepG2 cells (% viable after 16 h: >99%). XEN907 shows moderate hepatocyte stability (% remaining after 2 h: rat 21%; human 34%; dog 46%) across species |
| 体内研究： |
XEN907 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (13 %), Cmax (35 ng/mL), and AUClast (143 h•ng/mL) in rats. XEN907 (3 mg/kg; i.v.) exhibits terminal elimination half-life (2.6 h), high plasma clearance (9.4 L/h/kg), and large volumes of distribution (35.0 L/kg) in rats |
| 参考文献： |
1. Chowdhury S, et al. Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3676-81. 2. Chowdhury S, et, al. Tetracyclic spirooxindole blockers of hNaV1.7: activity in vitro and in CFA-induced inflammatory pain model. Med Chem Res (2013) 22:1825–1836. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.846 ml |
14.229 ml |
28.458 ml |
| 5 mM |
0.569 ml |
2.846 ml |
5.692 ml |
| 10 mM |
0.285 ml |
1.423 ml |
2.846 ml |
| 50 mM |
0.057 ml |
0.285 ml |
0.569 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
